Pharmacology: Insomnia Drugs and Treatments
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Questions and Answers

What is a recommended first-line approach for managing insomnia in children?

  • Pharmacologic therapy with antihistamines
  • Non-pharmacologic therapy (correct)
  • Cognitive-behavioral therapy
  • Sedative antidepressants

    • What potential risks are associated with using benzodiazepines during pregnancy?

  • Shortened labor duration
  • Higher birth weights
  • Increased risk of neonatal withdrawal symptoms (correct)
  • Reduced risk of oral clefts

    • Which of the following medications is indicated for treating sleep-maintenance insomnia in elderly patients?

  • Gabapentin
  • Lorazepam
  • Low-dose doxepin (correct)
  • Zopiclone

    • Which characteristic best differentiates sedative drugs from hypnotic drugs?

    <p>Sedatives reduce excitement, while hypnotics induce a state of sleep.</p> Signup and view all the answers

    What is the primary consideration when prescribing pharmacologic interventions for insomnia in pregnant women?

    <p>Severity and disabling nature of insomnia</p> Signup and view all the answers

    What is a key indication for the use of benzodiazepines in treating insomnia?

    <p>Sleep onset difficulties</p> Signup and view all the answers

    What is a noted concern when using antihistamines for insomnia treatment in pediatric patients?

    <p>Risk of rapid tolerance development</p> Signup and view all the answers

    Which off-label agent can be used for insomnia associated with fibromyalgia?

    <p>Anticonvulsants</p> Signup and view all the answers

    Which class of medication is most strongly associated with long-term dependence when used for insomnia?

    <p>Benzodiazepines</p> Signup and view all the answers

    What is the primary mechanism of action for Z-drugs such as Zopiclone?

    <p>Stimulates GABA related inhibition</p> Signup and view all the answers

    What is a potential consequence of polypharmacy in elderly patients with insomnia?

    <p>Increased risk of falls</p> Signup and view all the answers

    What distinguishes sedative drugs from hypnotic drugs in their use for insomnia?

    <p>Hypnotic drugs primarily induce sleep</p> Signup and view all the answers

    What percentage of individuals with insomnia are reported to have comorbid conditions contributing to their insomnia?

    <p>75%</p> Signup and view all the answers

    Which of the following medications is NOT typically associated with improving insomnia when used off-label?

    <p>Stimulants</p> Signup and view all the answers

    In what situation should the prescribing of insomnia medications be approached with caution?

    <p>For elderly patients</p> Signup and view all the answers

    What is the recommended duration for prescribing insomnia medications according to general principles?

    <p>30-60 days</p> Signup and view all the answers

    What is the recommended waiting period before patients can drive or operate machinery after taking sedative medications?

    <p>12 hours</p> Signup and view all the answers

    What is a common adverse effect associated with Z-drugs?

    <p>Complex sleep behaviors</p> Signup and view all the answers

    How do dual orexin antagonists function in regulating sleep?

    <p>By normalizing sleep-wake function</p> Signup and view all the answers

    Which characteristic distinguishes Z-drugs from benzodiazepines regarding adverse effects?

    <p>Less potential for rebound insomnia</p> Signup and view all the answers

    Which of the following is true regarding Doxepin used for insomnia?

    <p>It does not cause rebound insomnia.</p> Signup and view all the answers

    What type of adverse effects can increase when Z-drugs are combined with other CNS depressants?

    <p>Complex sleep behaviors</p> Signup and view all the answers

    What is a potential effect of benzodiazepine withdrawal?

    <p>Rebound insomnia</p> Signup and view all the answers

    What would be a primary reason to prefer Z-drugs over benzodiazepines for treating insomnia?

    <p>They have fewer adverse effects.</p> Signup and view all the answers

    Which condition is specifically contraindicated for dual orexin antagonists like Lemborexant?

    <p>Narcolepsy</p> Signup and view all the answers

    What is a significant benefit of Lemborexant compared to other sleep medications?

    <p>Minimal next-day impairment</p> Signup and view all the answers

    Which of the following is a primary reason benzodiazepines are recommended for short-term use only?

    <p>They may cause long-term dependence and withdrawal symptoms.</p> Signup and view all the answers

    What characteristic makes Temazepam the most suitable benzodiazepine according to recommendations?

    <p>It carries a Health Canada indication.</p> Signup and view all the answers

    Which of the following adverse effects is commonly associated with benzodiazepines?

    <p>Dose-dependent ataxia and dizziness.</p> Signup and view all the answers

    What is the risk of using benzodiazepines in conjunction with alcohol or other CNS depressants?

    <p>It may result in increased sedation and respiratory depression.</p> Signup and view all the answers

    What is a significant drawback of using Flurazepam and Nitrazepam as benzodiazepines for insomnia?

    <p>They have long half-lives leading to potential next-day impairment.</p> Signup and view all the answers

    Which of the following best describes the general approach to prescribing medication for insomnia with comorbidity?

    <p>Treat the underlying condition adequately before addressing the insomnia.</p> Signup and view all the answers

    What is the primary goal of therapy for insomnia?

    <p>To improve daytime functioning and reduce impairment.</p> Signup and view all the answers

    What is a common misconception regarding the use of antidepressants in insomnia treatment?

    <p>They can sometimes contribute to insomnia due to their stimulating effects.</p> Signup and view all the answers

    Which of the following medications is most likely to require cautious use due to the potential for dependence?

    <p>Benzodiazepines such as Temazepam.</p> Signup and view all the answers

    Which condition is NOT typically associated with insomnia comorbidity?

    <p>Chronic fatigue syndrome.</p> Signup and view all the answers

    What principle should guide the duration for which insomnia medications are prescribed?

    <p>Use the lowest effective dose for the shortest suitable duration.</p> Signup and view all the answers

    What factor is crucial to consider when using sedatives for insomnia in elderly patients?

    <p>Sedatives can lead to increased fall risk in this population.</p> Signup and view all the answers

    Which off-label use for insomnia might be appropriate for patients experiencing chronic pain?

    <p>Antidepressants to simultaneously address mood and sleep.</p> Signup and view all the answers

    What should be avoided when treating insomnia in elderly patients to reduce the risk of falls?

    <p>Medications causing sedation</p> Signup and view all the answers

    Which of the following conditions may not warrant pharmacologic treatment for insomnia in pregnant women?

    <p>Mild insomnia</p> Signup and view all the answers

    Which of the following is a potential risk associated with the off-label use of antihistamines for treating insomnia in children?

    <p>Next-day sedation</p> Signup and view all the answers

    In the context of insomnia treatment in those with concomitant pain conditions, which off-label agent is most commonly utilized?

    <p>Anticonvulsants</p> Signup and view all the answers

    What is a fundamental principle regarding the use of pharmacologic agents for treating insomnia in pediatric patients?

    <p>Limit medication use due to lack of evidence</p> Signup and view all the answers

    Which of the following interventions is the first line when addressing insomnia in pregnant women?

    <p>Non-pharmacologic options</p> Signup and view all the answers

    What main concern is there when prescribing sedative medications to elderly patients?

    <p>Increased risk of falls</p> Signup and view all the answers

    When considering treatment options for insomnia related to mood disorders, which medication class is often applied?

    <p>Sedating antidepressants</p> Signup and view all the answers

    What is a common adverse effect of Z-drugs?

    <p>Bitter/metallic taste</p> Signup and view all the answers

    Which of the following statements about Lemborexant is correct?

    <p>It is effective for sleep-onset and sleep maintenance insomnia.</p> Signup and view all the answers

    What is a key benefit of using Doxepin for insomnia treatment?

    <p>Reduced next-day impairment</p> Signup and view all the answers

    What characterizes the mechanism of action for benzodiazepine receptor agonists?

    <p>They enhance inhibition via GABA-A receptors.</p> Signup and view all the answers

    What should patients be advised against when taking Z-drugs or benzodiazepines?

    <p>Using alcohol or other CNS depressants</p> Signup and view all the answers

    What is a noted adverse effect associated with dual orexin antagonists?

    <p>Sleepwalking with memory loss</p> Signup and view all the answers

    Which statement best describes a particular nuance of Z-drugs compared to benzodiazepines?

    <p>Z-drugs have no potential for dependence.</p> Signup and view all the answers

    What is the result of long-term use of benzodiazepines for insomnia treatment?

    <p>Potential for rebound insomnia upon discontinuation</p> Signup and view all the answers

    Which of the following adverse effects is least commonly associated with Lemborexant?

    <p>Weight gain</p> Signup and view all the answers

    What differentiates Doxepin from other sleep medications regarding dependency and adverse effects?

    <p>Limited addictive potential</p> Signup and view all the answers

    Study Notes

    Pharmacology: Insomnia

    • Insomnia is defined as dissatisfaction with sleep quality or quantity, plus one or more of the following:
      • Difficulty falling asleep (sleep onset).
      • Difficulty staying asleep (sleep maintenance).
      • Early morning awakening without being able to return to sleep.

    Lecture Competencies

    • Compare and contrast the mechanisms of action, indications, and adverse effects of drugs to treat insomnia (with and without comorbidities).
      • Benzodiazepines (e.g., Temazepam).
      • Benzodiazepine receptor agonists (Z-drugs) (e.g., Zopiclone).
      • Dual orexin receptor antagonists (e.g., Lemborexant).
      • Tricyclic antidepressants (e.g., Doxepin).
    • Discuss drugs often used off-label for comorbid insomnia.
    • Discuss pharmacotherapeutic options for children.
    • Discuss pharmacotherapeutic options for the elderly.
    • Discuss pharmacotherapeutic options for use during pregnancy and breastfeeding.
    • Prescribe appropriate medications for people with insomnia based on patient history.

    Goals of Therapy

    • Improve daytime function.
    • Reduce daytime impairment (e.g., dysphoria, fatigue, decreased alertness).
    • Promote subjectively sound and restorative sleep.
    • Potentiate the effectiveness of behavioural interventions.

    Medications Contributing to Insomnia

    • Antidepressants
    • Stimulants
    • Antihypertensives
    • Sedatives
    • Decongestants and antihistamines
    • Analgesics
    • Herbal supplements
    • Substances of abuse

    Insomnia with Comorbidity

    • Many people with insomnia have other conditions that contribute to their sleep problems.
      • Musculoskeletal conditions.
      • Psychiatric disorders.
      • Respiratory disorders.
      • GI disorders.
      • Chronic pain.
    • Many insomnia medications were studied in individuals without comorbidities.
    • This has led to variable prescribing behaviours.

    General Principles

    • Use the lowest effective dose for the shortest duration.
    • Follow up frequently (3–6 weeks).
    • Dispense limited supplies (30–60 days).
    • Ensure the underlying condition is adequately treated for those with comorbid insomnia.

    Definitions

    • Sedative: A drug that reduces excitement and calms the patient. Also called anxiolytics. They do not induce sleep.
    • Hypnotic: A drug that results in drowsiness that promotes sleep.

    Benzodiazepines

    • GABA-A receptor agonists.
    • Enhance chloride ion movement through GABA receptors.
    • Enhance GABA channel effects and inhibition.
    • Have sedative and hypnotic properties, but differ in potency and pharmacokinetics.
    • Should only be used for short-term acute or intermittent insomnia.
    • Long-term use should only be considered in severe or comorbid insomnia when other treatments have failed.
    • Do not use multiple benzodiazepines (e.g., insomnia and anxiety).
    • Do not combine with alcohol or other CNS depressants.

    Benzodiazepine Properties (Table)

    Drug Equivalent Dose Onset of Action Average Half-Life
    Clonazepam 0.25 mg 20-60 min 34 (19-60) hr
    Flurazepam* 15 mg 30-60 min 100 (40-250) hr
    Lorazepam 1 mg 30-60 min 15 (8-24) hr
    Nitrazepam* 5 mg 10-40 min 16-48 hr
    Oxazepam 15 mg Slow 8 (3-25) hr
    Temazepam* 10 mg Slow 11 (3-25) hr
    Triazolam* 0.25 mg 15-30 min 2 (1.5-5) hr
    • *Officially indicated for insomnia in Canada.

    Benzodiazepines - Further Considerations

    • Flurazepam and nitrazepam are not recommended due to long half-lives.
    • Triazolam is not recommended due to high risk of abuse, dependence, and rebound insomnia.
    • Temazepam is suitable for those with Health Canada indications.

    Adverse Effects of Benzodiazepines

    • Dose-dependent ataxia, dizziness, dependence, withdrawal symptoms, impaired memory, risk of abuse.
    • May cause dose-dependent next-day impairment, even if the patient feels fully awake.
    • Use when there's a 7-8-hour period before awakening.
    • Advise patients to wait at least 12 hours before driving or operating machinery.

    Benzodiazepines - Use Duration

    • Have been studied for up to 24 weeks.
    • Rebound insomnia may occur after discontinuation.
    • Deprescribing/gradual tapering over months may help.

    Benzodiazepine Receptor Agonists (Z-Drugs)

    • Allosteric modulators of GABA-A receptors.
    • The presence of GABA does not facilitate action.
    • Similar mechanism to benzodiazepines, where enhanced inhibition is caused via GABA-A receptors.

    Z-Drugs - Benefits

    • Generally the preferred class for treating insomnia.
    • Similar effect on sleep to benzodiazepines.
    • Fewer adverse effects.
    • Less muscle relaxant effects.
    • Do not worsen sleep apnea.
    • Does not accumulate; less rebound on withdrawal.

    Z-Drugs - Specifics

    • Zopiclone is the most common Z-drug prescribed in Canada.

    Adverse Effects of Z-Drugs

    • Bitter/metallic taste, dry mouth, dizziness, somnolence.
    • Complex sleep behaviours (night eating, somnambulism).
    • May cause dose-dependent next-day impairment of activities requiring alertness (e.g., driving).
    • Use only when there's a 7-8-hour period before planned awakening.
    • Avoid combining with alcohol or other CNS depressants. Increased risk of complex sleep behaviours if combined with other CNS-active drugs.

    Dual Orexin Antagonists

    • Orexin/receptor pathways play vital regulatory roles (e.g., feeding behaviour, sleep-wake rhythm, reward, etc.).
    • Neuropeptides in the hypothalamus promote arousal/wakefulness.
    • Lemborexant is a competitive dual orexin antagonist.
    • Normalizes sleep-wake function, reduces unwanted transitions.

    Lemborexant -Further Considerations

    • No evidence of withdrawal symptoms or rebound insomnia.
    • Evidence supports efficacy for up to 12 months.
    • Minimal next-day impairment.
    • Minimal abuse potential.

    Adverse Effects of Lemborexant

    • Somnolence.
    • Less commonly: sleep paralysis, hypnagogic/hypnopompic hallucinations, cataplexy-like symptoms.
    • Complex sleep behaviours (night eating, somnambulism).
    • May cause dose-dependent next-day impairment of activities requiring alertness (driving).
    • Use only when there's a 7-8-hour period before planned awakening.
    • Limited effects on driving impairment after 9 hours.
    • Avoid combining with other CNS depressants.
    • Contraindicated in narcolepsy.

    Tricyclic Antidepressants (Doxepin)

    • Selective histamine H1 receptor antagonist at low dosages.
    • H1 receptors are associated with arousal and waking in the brain.
    • Agonists promote wakefulness, antagonists promote sleep.

    Doxepin -Further Considerations

    • Indicated by Health Canada for sleep-maintenance difficulties.
    • Trials support use for up to 3 months.
    • May improve sleep maintenance better than GABA-A agonists.
    • Not associated with rebound insomnia, dependence, or next-day impairment.
    • Recommended treatment for the elderly.

    Adverse Effects of Doxepin

    • At low dosages, typical adverse effects are not seen.
    • Somnolence, sedation, nausea may occur at higher doses..
    • Should not be combined with alcohol or other CNS depressants.
    • Should not be taken within 3 hours of food.

    Off-Label Agents

    • Many drugs causing sedation are sometimes used for conditions other than insomnia (off-label).
    • Goal is to treat an underlying comorbidity while promoting sleep.
    • Limited evidence for this practice.

    Specific Examples of Off-Label Agents

    • Insomnia with Centralized pain (e.g. fibromyalgia).
    • Anticonvulsants (e.g. gabapentin).
    • Conditions with allergy (e.g, eczema or allergies).
    • Antihistamines.
    • Insomnia and mood disorders.
    • Antidepressants (sedating).

    Insomnia and Children

    • Non-pharmacological therapy generally recommended as first-line treatment.
    • Limited evidence to guide use of medications.
    • Over-the-counter antihistamines are not recommended, due to potential for rapid tolerance, next-day sedation, impaired cognitive function, and paradoxical reactions.
    • Drugs should target the comorbidity.

    Insomnia and the Elderly

    • Prone to polypharmacy and drug interactions.
    • Limit sedation-causing drugs to reduce fall risk.
    • Recommend low-dose doxepin or Lemborexant
    • Lemborexant suitable up to 6 months.

    Insomnia and Pregnancy

    • Disrupted sleep is a common complaint.
    • Sleep apnea and restless leg syndrome can worsen during pregnancy.
    • Little research on insomnia during pregnancy.
    • No controlled studies of interventions in this population.
    • Non-pharmacological options are generally first-line.
    • Consider risk-benefit ratio for patients and developing fetus with pharmacologic interventions.
    • Zopiclone can be a reasonable option. Avoid benzodiazepines particularly early in pregnancy

    Case Studies (brief summaries)

    • Case #1: 72-year-old with fatigue (frequent urination, potential hypertension/dyslipidemia).
    • Case #2: 47-year-old with alcohol use disorder and daytime sleepiness (sleep disturbance history).

    Case Study Considerations (brief examples)

    • Case #1: Consider the patient's age, existing medications, potential medication interactions, and best drug option for insomnia.
    • Case #2: Consider underlying diagnosis, type of insomnia, alcohol use considerations, and best treatment options.

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    Pharmacology: Insomnia PDF

    Description

    This quiz covers the pharmacological treatments for insomnia, including their mechanisms of action, indications, and adverse effects. It examines various drug classes such as benzodiazepines, Z-drugs, and tricyclic antidepressants, as well as considerations for special populations like children and the elderly. Test your knowledge on effective insomnia therapies!

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